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Chemical Compound Review

TILETAMINE     2-ethylamino-2-thiophen-2-yl- cyclohexan-1-one

Synonyms: Tiletamina, Tiletaminum, SureCN115212, cc-428, BSPBio_001203, ...
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Disease relevance of CI-634

  • Seven atopic dogs underwent intradermal allergy testing with 46 inhalant antigens before and after administration of a tiletamine/zolazepam solution (4 mg/kg of body weight, IV) [1].
  • Aerophaia and gastric dilation following tiletamine/zolazepam anaesthesia in a dog [2].
  • CONCLUSIONS AND CLINICAL RELEVANCE: Tiletamine/zolazepam injection may induce transient hypoxaemia and respiratory acidosis, but acid-base status changes are clinically unimportant [3].
  • Mild nephrosis was present in three of four rabbits injected with 7.5 mg/kg of tiletamine [4].

High impact information on CI-634


Chemical compound and disease context of CI-634


Biological context of CI-634

  • In Mg++-free perfusate, the excitatory postsynaptic potential was greatly augmented to give a paroxysmal depolarization shift and was reversibly blocked by 10 microM tiletamine [8].
  • In striatal slices, tiletamine inhibited the NMA-mediated, but not the spontaneous, release of [3H]acetylcholine, with an IC50 of 70 nM [8].
  • The convulsant effect of tiletamine and its excitatory effect on spinal H-reflexes at higher doses, however, appear to be mediated by non-NMDA receptors [10].
  • All animals were anesthetized using a zolazepam + tiletamine mixture injected intramuscularly; heart rate and rectal temperature were monitored and corneal irrigation was regularly performed [11].
  • Chemical immobilization of adult female Weddell seals with tiletamine and zolazepam: effects of age, condition and stage of lactation [12].

Anatomical context of CI-634

  • Tiletamine is a potent inhibitor of N-methyl-aspartate-induced depolarizations in rat hippocampus and striatum [8].
  • Our results show that tiletamine is a potent and reversible antagonist of NMA-mediated responses without itself having major effects in low concentrations on normal membrane and synaptic pyramidal cell properties [8].
  • (tiletamine chloridrate 125.0 mg and zolazepan chloridrate 125.0 mg) into quadriceps muscle intramuscularly (IM), saliva was collected using pre-weighed small cotton balls inserted in the animal's mouth [13].

Associations of CI-634 with other chemical compounds


Gene context of CI-634

  • It is concluded that the anticonvulsant and reflex suppressant action of tiletamine are due to antagonism of NMDA receptor-mediated excitation [10].
  • Injection-site tissue concentrations were determined to be 25.1 mg/kg tiletamine and 23.3 mg/kg for zolazepam [19].

Analytical, diagnostic and therapeutic context of CI-634


  1. Effect of tiletamine/zolazepam sedation on intradermal allergy testing in atopic dogs. Codner, E.C., Lessard, P., McGrath, C.J. J. Am. Vet. Med. Assoc. (1992) [Pubmed]
  2. Aerophaia and gastric dilation following tiletamine/zolazepam anaesthesia in a dog. Savas, I., Plevraki, K., Raptopoulos, D. Vet. Rec. (2001) [Pubmed]
  3. Blood gas and acid-base status during tiletamine/zolazepam anaesthesia in dogs. Savvas, I., Plevraki, K., Raptopoulos, D., Koutinas, A.F. Veterinary anaesthesia and analgesia. (2005) [Pubmed]
  4. Nephrotoxicity of tiletamine in New Zealand white rabbits. Doerning, B.J., Brammer, D.W., Chrisp, C.E., Rush, H.G. Lab. Anim. Sci. (1992) [Pubmed]
  5. Induction of hepatic cytochrome P450 2B and P450 3A isozymes in rats by zolazepam, a constituent of Telazol. Wong, A., Bandiera, S.M. Biochem. Pharmacol. (1998) [Pubmed]
  6. Inductive effect of Telazol on hepatic expression of cytochrome P450 2B in rats. Wong, A., Bandiera, S.M. Biochem. Pharmacol. (1996) [Pubmed]
  7. Slow and saccadic eye movements evoked by microstimulation in the supplementary eye field of the cebus monkey. Tian, J.R., Lynch, J.C. J. Neurophysiol. (1995) [Pubmed]
  8. Tiletamine is a potent inhibitor of N-methyl-aspartate-induced depolarizations in rat hippocampus and striatum. ffRench-Mullen, J.M., Lehmann, J., Bohacek, R., Fisher, R.S. J. Pharmacol. Exp. Ther. (1987) [Pubmed]
  9. Anesthesia of wood bison with medetomidine-zolazepam/tiletamine and xylazine-zolazepam/tiletamine combinations. Caulkett, N.A., Cattet, M.R., Cantwell, S., Cool, N., Olsen, W. Can. Vet. J. (2000) [Pubmed]
  10. Paradoxical convulsant action of a novel non-competitive N-methyl-D-aspartate (NMDA) antagonist, tiletamine. Klockgether, T., Turski, L., Schwarz, M., Sontag, K.H., Lehmann, J. Brain Res. (1988) [Pubmed]
  11. SLO angiography: arterio-venous filling times in monkey and minipig. Rosolen, S.G., Saint-Macary, G., Gautier, V., Le Gargasson, J.F. Veterinary ophthalmology. (2002) [Pubmed]
  12. Chemical immobilization of adult female Weddell seals with tiletamine and zolazepam: effects of age, condition and stage of lactation. Wheatley, K.E., Bradshaw, C.J., Harcourt, R.G., Davis, L.S., Hindell, M.A. BMC Vet. Res. (2006) [Pubmed]
  13. Moxonidine and rilmenidine injected into the medial septal area reduces the salivation induced by pilocarpine. Saad, W.A., de Arruda Camargo, L.A., Simões, S., Saad, W.A., Guarda, R.S., Guarda, I.F. Autonomic neuroscience : basic & clinical. (2004) [Pubmed]
  14. A fatality related to the veterinary anesthetic telazol. Cording, C.J., DeLuca, R., Camporese, T., Spratt, E. Journal of analytical toxicology. (1999) [Pubmed]
  15. Effects of tiletamine/zolazepam premedication on propofol anaesthesia in dogs. Cullen, L.K., Reynoldson, J.A. Vet. Rec. (1997) [Pubmed]
  16. The use of tiletamine hydrochloride and zolazepam hydrochloride for sedation of the mountain brushtial possum, Trichosurus caninus Ogilby (Phalangeridae: Marsupialia). Viggers, K.L., Lindenmayer, D.B. Aust. Vet. J. (1995) [Pubmed]
  17. Chemical immobilization of crested porcupines with tiletamine HCl and zolazepam HCl (Zoletil) under field conditions. Massolo, A., Sforzi, A., Lovari, S. J. Wildl. Dis. (2003) [Pubmed]
  18. Immobilization of babirusa (Babyrousa babyrussa) with xylazine and tiletamine/zolazepam and reversal with yohimbine and flumazenil. James, S.B., Cook, R.A., Raphael, B.L., Stetter, M.D., Kalk, P., MacLaughlin, K., Calle, P.P. J. Zoo Wildl. Med. (1999) [Pubmed]
  19. A fatality due to injection of tiletamine and zolazepam. Chung, H., Choi, H., Kim, E., Jin, W., Lee, H., Yoo, Y. Journal of analytical toxicology. (2000) [Pubmed]
  20. Tiletamine and zolazepam for immobilization of wild lions and leopards. King, J.M., Bertram, B.C., Hamilton, P.H. J. Am. Vet. Med. Assoc. (1977) [Pubmed]
  21. Evaluation of use of tiletamine/zolazepam for anesthesia of bullfrogs and leopard frogs. Letcher, J., Durante, R. J. Am. Vet. Med. Assoc. (1995) [Pubmed]
  22. Removal of the OptEase retrievable vena cava filter is not feasible after extended time periods because of filter protrusion through the vena cava. Ashley, D.W., Mix, J.W., Christie, B., Burton, C.G., Lochner, F.K., McCommon, G.W., Matoy, G.C., Solis, M.M., Donner, R.S., Dalton, M.L., Tyson, C.S., Newman, W.H. The Journal of trauma. (2005) [Pubmed]
  23. Epidural administration of tiletamine/zolazepam in horses. Natalini, C.C., Alves, S.D., Guedes, A.G., Polydoro, A.S., Brondani, J.T., Bopp, S. Veterinary anaesthesia and analgesia. (2004) [Pubmed]
  24. Oral induction of anesthesia with droperidol and transmucosal carfentanil citrate in chimpanzees (Pan troglodytes). Kearns, K.S., Swenson, B., Ramsay, E.C. J. Zoo Wildl. Med. (2000) [Pubmed]
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